Iran Polymer and Petrochemical Institute, P,O, Box:14185/458, Tehran, Iran.
Daru. 2013 Jul 15;21(1):57. doi: 10.1186/2008-2231-21-57.
A poly (lactide-co-glycolide) (PLGA) implant was used to control the release profile of leuprolide acetate (LA) drug. The system is an in-situ polymeric precipitation system. And the formulation consisted of PLGA polymer, LA drug and N-methyl-2-pyrrolidon solvent with no additives. First, the formulation was injected into PBS solution for in-vitro studies and then it was administered to the animal models (female rats) for in-vivo release studies. The release profiles of leuprolide acetate were measured by UV spectrophotometry for a period of 28 days. The initial burst release of LA was 14% in in-vitro whereas it was 7% in in-vivo. In-vitro and in-vivo release profiles of LA had similar trends after 72 hours. However, the rate of LA release was slower in-vivo. This might be attributed to the limited diffusion process of solvent and the drug molecules. This could be due to presence of an additional pressure caused by the surrounding tissue and also the presence of small amount of water between cells in the subcutaneous site. Cross-section and surface of the implants were studied via scanning electron microscopy. Morphology of both in-vitro and in-vivo implants confirmed the release behaviours. No toxicity effects were reported in the histopathological assay. Furthermore, the pharmacological analysis showed more inactive ovaries due to release of LA.
聚（乳酸-共-乙醇酸）（PLGA）植入物用于控制醋酸亮丙瑞林（LA）药物的释放曲线。该系统是一种原位聚合沉淀系统。制剂由 PLGA 聚合物、LA 药物和 N-甲基-2-吡咯烷酮溶剂组成，没有添加剂。首先，将制剂注入 PBS 溶液中进行体外研究，然后将其施用于动物模型（雌性大鼠）进行体内释放研究。通过紫外分光光度法测定醋酸亮丙瑞林的释放曲线，持续 28 天。体外初始突释为 14%，而体内为 7%。72 小时后，LA 的体外和体内释放曲线具有相似的趋势。然而，体内 LA 的释放速度较慢。这可能归因于溶剂和药物分子的扩散过程有限。这可能是由于周围组织产生的额外压力以及在皮下部位细胞之间存在少量水的原因。通过扫描电子显微镜研究了植入物的横截面和表面。体外和体内植入物的形态学证实了释放行为。组织病理学分析未报告任何毒性作用。此外，药理分析表明由于 LA 的释放，卵巢的活性降低。
